Eglumegad-LY354740-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEglumegadCat. No.: HY-18941CAS No.: 176199-48-7Synonyms: LY354740; Eglumetad分式: CHNO分量: 185.18作靶点: mGluR作通路: GPCR/G Protein; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 H2O :

2、 6.33 mg/mL (34.18 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 5.4002 mL 27.0008 mL 54.0015 mL5 mM 1.0800 mL 5.4002 mL 10.8003 mL10 mM 0.5400 mL 2.7001 mL 5.4002 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Eglumegad (LY354740)种有效，选择性的 g

3、roup II (mGlu2/3) receptor 激动剂，对mGlu2和mGlu3受体的 IC50 分别为5和24 nM。体外研究Eglumegad (LY354740) down-regulates spots 1014, 1822 (hypoxia up-regulated protein 1), 4513 (an isoformof protein disulfide isomerase 3), 6204, 6312, 7306 (26S proteasome non-ATPase regulatory subunit 7) andprotein spots 1013 and 600

4、5 (destrin), and up-regulates spot 6507 (collapsin response mediator protein 1) in1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEmouse cortical neurons 2.体内研究 Eglumegad (LY354740) (15 or 30 mg/kg, i.p.) has no effect on spatial working memory performance inGria1/ or WT mice, and it has no effect o

5、n rewarded alternation testing with a short inter-trial interval inGria1/ and WT mice at concentration of 30 mg/kg. Eglumegad (LY354740) (15 or 30 mg/kg, i.p.) reducesspontaneous locomotor activity in wild-type and Gria1/ mice 1. Eglumegad (LY354740) (15 mg/kg, i.p.)dreases novelty-induced hyperloco

6、motion in naive GluA1-KO and pre-handled GluA1-KO males, but not infemales. Eglumegad (LY354740) (15 mg/kg, i.p.) significantly reduces the increased c-Fos expression ofGluA1-KO males to the level of WT males, but not in of females 3. Eglumegad (LY354740) (10 mg/kg, i.p.)attenuates the immobilizatio

7、n stress-induced increase in BDNF mRNA expression in the rat mPFC 4.PROTOCOLAnimal Mice 1Administration 14 In Experiment 1A wild-type (female: N=6; male: N=5) and Gria1/ mice (female: N=7; male: N=8) firstreceive 30 trials of drug-free testing (five trials per day for 6 days). Each animal is then te

8、sted on rewardedalternation following an injection of either Eglumegad (LY354740) (15 mg/kg) or vehicle. After injectionanimals are returned to the home cage for 30 min before behavioural testing commenced. Each animal isgiven 10 trials of rewarded alternation in the T-maze. Mice are given a maximum

9、 of 120 s to a complete atrial. At least 24 h after the first round of drug testing the animals are re-tested in the absence of any drugtreatment to ensure that there are no long-term effects of the drug, and that the mice maintain a high level ofalternation performance. Twenty-four hours after this

10、 re-testing, mice receive a further 10 trials of rewardedalternation testing, but now under the drug condition that they have not previously received. The order ofdrug exposure is counterbalanced within genotype and sex as far as possible given the numbers of mice. Inall stages, the number of trials

11、 in which the animal alternated, as well as time taken to run from the start armto the food well on the sample run (sample latency), and the time taken to run from the start arm to making achoice on the choice run (choice latency), are recorded. Latencies are measured by the experimenter using astop

12、watch. The experimenter is blind to the genotype and drug allocations of the animals throughout testing.In Experiment 1B, separate groups of male wild-type (N=7) and Gria1/ mice (N=7) undgo the sameprocedure as Experiment 1A but now they receive either vehicle or a higher dose of Eglumegad (LY354740

13、)(30 mg/kg). Subsequently, in Experiment 1C, to investigate the potential effects of increased proactiveinterference, the procedure used in Experiment 1B is repeated in the same mice, using the same drug dose(30 mg/kg), but now using a modified testing protocol in which the interval between trials i

14、s reduced to 20 s.Rats 4Two experiments are conducted. The first experiment compares the effects of LY354740 (10 mg/kg, i.p.,neutralized to a pH 7.4) or vehicle (0.9% saline neutralized to pH 7.4) in rats remaining in their homecages or rats exposed to 2 h of immobilization stress in plastic cones (

15、n=7, cage control/vehicle; n=7, cagecontrol/LY354740; n=6, stress/vehicle; n=6, stress/Eglumegad (LY354740). The second experimentcompares two lower LY354740 doses (1 and 3 mg/kg, i.p.) or vehicle in rats exposed to a 2-h period ofimmobilization stress to rats treated with vehicle in their home cage

16、s (n=4 for all groups). All animals areinjected with either Eglumegad (LY354740) or vehicle 15 min prior to being placed in plastic cones with theopen end securely closed. All immobilized rats are placed in plexiglass chamber with animal bedding on thebottom; brought to a quiet room outside of the a

17、nimal colony; and immediately placed in a plastic cone. Two2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEhours after being placed in the plastic containers, the rats are decapitated. The brains are removed andfrozen on dry ice, and stored at 80C.MCE has not independently confirmed the accuracy of

18、 these methods. They are for reference only.REFERENCES1. Boerner T, et al. The group II metabotropic glutamate receptor agonist LY354740 and the D2 receptor antagonist haloperidol reducelocomotor hyperactivity but fail to rescue spatial working memory in GluA1 knockout mice. Eur J Neurosci. 2017 Apr;45(7):912-2. Orlando R, et al. Levels of the Rab GDP dissociation inhibitor (GDI) are altered in the prenatal restrain stress mouse model ofschizophrenia and are differentially regulated by the mGlu2/3 receptor agonists, LY379268 and LY354740.